Synthesis and antitumor activity of novel 6-aryl and 6-alkylpyrazolo[3,4- d]pyrimidin-4-one derivatives

• Published in: European journal of medicinal chemistry Vol. 45; no. 11; pp. 5286 - 5291
• Main Authors: El-Enany, Mervat M., Kamel, Mona M., Khalil, Omneya M., El-Nassan, Hala B.
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 01.11.2010; Elsevier
• Subjects: Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Antitumor activity; Biological and medical sciences; Cell Line, Tumor; Chemistry, Medicinal; Drug Screening Assays, Antitumor; General aspects; HCT116; Humans; Inhibitory Concentration 50; Life Sciences & Biomedicine; Magnetic Resonance Spectroscopy; Medical sciences; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Pyrazolo[3,4- d]pyrimidin-4-one; Pyrimidinones - chemical synthesis; Pyrimidinones - pharmacology; Science & Technology; Spectrophotometry, Infrared; Antitumor activity; HCT116; Pyrazolo[3,4- d]pyrimidin-4-one; Pyrazolo[3,4-d]pyrimidin-4-one; POTENT; INHIBITORS; ANTICANCER; Antineoplastic agent; Human; Solid tumor; Nitrogen heterocycle; Benzene derivatives; Cytotoxicity; In vitro; Pyrazolopyrimidine derivatives; Cell line; Structure activity relation; Bicyclic compound; Colon; Chemical synthesis; Tumor cell
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2010.08.048

A series of new 6-arylpyrazolo[3,4- d]pyrimidin-4-ones and 6-alkylpyrazolo[3,4- d]pyrimidin-4-ones were synthesized. Some of the newly synthesized compounds were tested in vitro on human colon tumor cell line (HCT116). Most of the test compounds exploited potent antitumor activity, especially compound 10a which displayed the highest activity among the test compounds with IC 50 equal to 0.47 μg/mL [Display omitted]